A series of C6-substituted N-hydroxy-2-quinolineacrylamides (3-15), with four types of bridging groups have been synthesized. Most of these compounds exhibit antiproliferative activity against A549 and HCT116 cells and Western blot analysis revealed that they are able to inhibit HDAC. Measurement of the HDAC isoform activity of ether-containing compounds showed that compound 9 has distinct HDAC6 selectivity, more than 300-fold over other isoforms. This paper describes the development of 6-aryloxy-N-hydroxy-2-quinolineacrylamides as potential HDAC6 inhibitors.

中文翻译：

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2-喹啉丙烯酰胺的合成及生物学评价。

合成了一系列具有四种桥联基团的一系列C6取代的N-羟基-2-喹啉丙烯酰胺（3-15）。这些化合物大多数对A549和HCT116细胞具有抗增殖活性，蛋白质印迹分析表明它们能够抑制HDAC。含醚化合物的HDAC同工型活性的测量表明，化合物9具有独特的HDAC6选择性，是其他同工型的300倍以上。本文介绍了作为潜在HDAC6抑制剂的6-芳氧基-N-羟基-2-喹啉丙烯酰胺的开发。